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Assay Detail

CHEMBL950281

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
Ghirmai S, Azar MR, Polgar WE, Berzetei-Gurske I, Cashman JR.
J Med Chem (2008) 51 : 1913 -1924
PubMed 18298057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.90 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272215 1 9.10
CHEMBL409458 1 8.85
CHEMBL429588 1 8.68
CHEMBL410122 1 8.56
CHEMBL410526 1 8.42
CHEMBL407466 1 8.37
CHEMBL429929 1 8.23
CHEMBL411738 1 8.17
CHEMBL438413 1 8.09
CHEMBL411916 1 8.07
CHEMBL271815 1 8.01
CHEMBL412050 1 7.91
CHEMBL271797 1 7.91
CHEMBL982 NALMEFENE 4.0 1 7.88
CHEMBL273105 1 7.80
CHEMBL19019 NALTREXONE 4.0 1 7.79
CHEMBL271811 1 7.75
CHEMBL270918 1 7.70
CHEMBL406116 1 7.61
CHEMBL271755 1 7.60
CHEMBL410884 1 7.57
CHEMBL411927 1 7.55
CHEMBL443326 1 7.49
CHEMBL272051 1 7.44
CHEMBL272181 1 7.43
CHEMBL260528 1 7.25
CHEMBL272021 1 7.10
CHEMBL409036 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272215 Ki = 0.79 nM 9.10
CHEMBL409458 Ki = 1.4 nM 8.85
CHEMBL429588 Ki = 2.07 nM 8.68
CHEMBL410122 Ki = 2.73 nM 8.56
CHEMBL410526 Ki = 3.8 nM 8.42
CHEMBL407466 Ki = 4.23 nM 8.37
CHEMBL429929 Ki = 5.82 nM 8.23
CHEMBL411738 Ki = 6.83 nM 8.17
CHEMBL438413 Ki = 8.22 nM 8.09
CHEMBL411916 Ki = 8.5 nM 8.07
CHEMBL271815 Ki = 9.72 nM 8.01
CHEMBL412050 Ki = 12.2 nM 7.91
CHEMBL271797 Ki = 12.4 nM 7.91
CHEMBL982 NALMEFENE Ki = 13.26 nM 7.88
CHEMBL273105 Ki = 15.8 nM 7.80
CHEMBL19019 NALTREXONE Ki = 16.31 nM 7.79
CHEMBL271811 Ki = 17.59 nM 7.75
CHEMBL270918 Ki = 19.91 nM 7.70
CHEMBL406116 Ki = 24.52 nM 7.61
CHEMBL271755 Ki = 25.29 nM 7.60
CHEMBL410884 Ki = 27.18 nM 7.57
CHEMBL411927 Ki = 28.0 nM 7.55
CHEMBL443326 Ki = 32.4 nM 7.49
CHEMBL272051 Ki = 36.52 nM 7.44
CHEMBL272181 Ki = 36.94 nM 7.43
CHEMBL260528 Ki = 56.3 nM 7.25
CHEMBL272021 Ki = 79.23 nM 7.10
CHEMBL409036 Ki = 99.0 nM 7.00